ES2637245T3 - Nuevas 4-(amino sustituido)-7H-pirrolo[2,3-d]pirimidinas como inhibidores de LRRK2 - Google Patents
Nuevas 4-(amino sustituido)-7H-pirrolo[2,3-d]pirimidinas como inhibidores de LRRK2 Download PDFInfo
- Publication number
- ES2637245T3 ES2637245T3 ES13752678.6T ES13752678T ES2637245T3 ES 2637245 T3 ES2637245 T3 ES 2637245T3 ES 13752678 T ES13752678 T ES 13752678T ES 2637245 T3 ES2637245 T3 ES 2637245T3
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- Prior art keywords
- pyrrolo
- pyrimidin
- procedure
- morpholin
- pyrimidine
- Prior art date
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- -1 4- (substituted amino) -7H-pyrrolo [2,3-d] pyrimidines Chemical class 0.000 title abstract description 47
- 229940124786 LRRK2 inhibitor Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract description 80
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract description 23
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 abstract description 14
- 125000005842 heteroatom Chemical group 0.000 abstract description 13
- 229910052757 nitrogen Inorganic materials 0.000 abstract description 12
- 229910052760 oxygen Inorganic materials 0.000 abstract description 12
- 229910052717 sulfur Inorganic materials 0.000 abstract description 11
- 125000001072 heteroaryl group Chemical group 0.000 abstract description 7
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract description 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract description 6
- 239000001257 hydrogen Substances 0.000 abstract description 6
- 229910052739 hydrogen Inorganic materials 0.000 abstract description 6
- 125000000753 cycloalkyl group Chemical group 0.000 abstract description 5
- 125000005843 halogen group Chemical group 0.000 abstract description 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract description 3
- 150000003839 salts Chemical class 0.000 abstract description 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract description 2
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract description 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract description 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
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- 238000000034 method Methods 0.000 description 210
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- 125000003821 2-(trimethylsilyl)ethoxymethyl group Chemical group [H]C([H])([H])[Si](C([H])([H])[H])(C([H])([H])[H])C([H])([H])C(OC([H])([H])[*])([H])[H] 0.000 description 7
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- QNXXNOAXMRJFPK-UHFFFAOYSA-N formic acid 4-[5-(1H-pyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]morpholine Chemical compound OC=O.C1CN(CCO1)c1ncnc2[nH]cc(-c3cn[nH]c3)c12 QNXXNOAXMRJFPK-UHFFFAOYSA-N 0.000 description 6
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- C—CHEMISTRY; METALLURGY
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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| US201361820828P | 2013-05-08 | ||
| PCT/IB2013/055039 WO2014001973A1 (fr) | 2012-06-29 | 2013-06-19 | Nouvelles 7h-pyrrolo[2,3-d]pyrimidines substituées par un groupe amino en position 4, utilisées comme inhibiteurs de lrrk2 |
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| EP (2) | EP3255049A1 (fr) |
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| CN (2) | CN105732639A (fr) |
| AP (1) | AP3902A (fr) |
| AR (1) | AR091628A1 (fr) |
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| CL (1) | CL2014003566A1 (fr) |
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| PH (1) | PH12014502886A1 (fr) |
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